共查询到20条相似文献,搜索用时 15 毫秒
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合成了3种含姜黄素衍生物(L1~L3)和1,3,5-三氮杂-7-磷金刚烷(PTA)配体的芳基钌配合物[(η6-p-cymene)Ru(L)(PTA)]PF6(1~3,L=L1~L3),通过X射线单晶衍射、核磁共振波谱、高分辨质谱、元素分析等方法表征了这些配合物的结构,并用MTT法研究了它们在λ>400 nm的光照辅助下对Hep G2人肝癌细胞的增殖抑制活性。结果表明,这3个配合物均为半三明治型结构;光辅助下,配合物抗癌活性明显提高,其中配合物3对HepG2细胞的IC50值从(60.3±1.1)μmol·L-1降低至(45.0±6.1)μmol·L-1。说明光照可以有效提高此类配合物的抗肿瘤活性。 相似文献
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合成了3种含姜黄素衍生物(L1~L3)和1,3,5-三氮杂-7-磷金刚烷(PTA)配体的芳基钌配合物[(η6-p-cymene)Ru(L)(PTA)]PF6(1~3,L=L1~L3),通过X射线单晶衍射、核磁共振波谱、高分辨质谱、元素分析等方法表征了这些配合物的结构,并用MTT法研究了它们在λ>400 nm的光照辅助下对HepG2人肝癌细胞的增殖抑制活性。结果表明,这3个配合物均为半三明治型结构;光辅助下,配合物抗癌活性明显提高,其中配合物3对HepG2细胞的IC50值从(60.3±1.1)μmol·L-1降低至(45.0±6.1)μmol·L-1。说明光照可以有效提高此类配合物的抗肿瘤活性。 相似文献
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Substitution‐Inert Polynuclear Platinum Complexes That Inhibit the Activity of DNA Polymerase in Triplex‐Forming Templates 下载免费PDF全文
Dr. Jaroslav Malina Prof. Nicholas P. Farrell Prof. Viktor Brabec 《Angewandte Chemie (International ed. in English)》2018,57(28):8535-8539
The formation of triple‐helical DNA is implicated in the regulation of gene expression. The triplexes are, however, unstable under physiological conditions so that effective stabilizers for the triplex formation are needed. Herein, we describe a new strategy for the stabilization of such triplexes that is based on antitumor substitution‐inert polynuclear platinum complexes (SI‐PPCs). These compounds were previously shown to bind to DNA through the phosphate clamp—a discrete mode of DNA–ligand recognition distinct from the canonical intercalation and minor‐groove binding. We have found that SI‐PPCs efficiently inhibit DNA synthesis by DNA polymerase in sequences prone to the formation of pyrimidine‐ and purine‐motif triplex DNAs. Moreover, the results suggest that SI‐PPCs are able to induce the formation of triple‐helical DNA between duplexes and strands that are not completely complementary to each other. Collectively, these data provide evidence that SI‐PPCs are very efficient stabilizers of triple‐stranded DNA that might exert their action by stabilizing higher‐order structures such as triple‐helical DNA. 相似文献
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临床使用的现代药物超过50%都来自于天然产物,它们不仅能够通过阻止细胞周期进程、抑制癌细胞存活信号通路以及调节免疫细胞等多种生物途径来阻止肿瘤生长及其进程,而且对正常组织表现出较低的毒性。虽然以顺铂为代表的金属抗肿瘤药物广泛用于临床,但是它们存在严重的耐药性和毒副作用,包括肾毒性、神经毒性等。因此,利用天然产物中的优势来改造铂类配合物,有望开发出新型铂类抗癌药物以克服铂药的缺陷。另一方面,芳基金属配合物因其良好的水溶性和对正常组织的低毒性受到了广泛关注,将天然产物与芳基金属配合物相结合,也为开发高效低毒的新型抗癌药物提供了更多可能。结合天然产物和金属各自优势开发基于天然产物的金属配合物作为抗癌剂已成为研究热点,开辟了抗癌的新途径。本文对已经报道的有关天然产物的铂类和芳基金属配合物的研究及作用机理进行了较为全面的综述,并对该领域的未来发展进行了展望。 相似文献
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Wan‐Jung Lin Dr. Abbas Raja Naziruddin Yu‐Hsuan Chen Dr. Bian‐Jian Sun Prof. Dr. A. Hsiu Hwa Chang Prof. Dr. Wen‐Jwu Wang Prof. Dr. Wen‐Shu Hwang 《化学:亚洲杂志》2015,10(3):728-739
Photoactive platinum complexes of stoichiometry [Pt(RCCCR)L]0/+ (R=Me, nBu and L=? CN, ? C≡CPh, ? N≡CCH3, ? Py, ? CO) featuring pincer‐type bis N‐heterocyclic carbene (NHC) ligands (RCCCR) were synthesized. Organometallic syntheses of these complexes are facile and achievable through standard laboratory procedures. Control of intermolecular Pt???Pt interaction, π–π stacking, and emission tuning is achieved through suitable choice of the NHC‐wingtip substituent (R) and the auxiliary ligand (L). Exposure to specific volatile organic compounds (VOCs) or mechanical grinding triggers changes in emission colors, which render these complexes photofunctional. Solid‐state structures and photoluminescence results are described herein. 相似文献
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肿瘤已成为严重威胁人类健康的重大疾病之一。以顺铂为首的铂类抗肿瘤药物一直是化疗首选药物。但是长期用药导致的一系列的毒副作用如肾毒性、耳毒性和耐药性等极大地限制了铂类配合物的发展与应用。本文针对目前铂类药物所处形势重点综述了新一代铂类药物的设计研发方法:(1)研发具有新颖结构的铂类药物,例如经过改造的反式铂类配合物、多核铂类配合物、Pt(Ⅳ)配合物等;(2)发展新的抗肿瘤靶点,例如以G-四螺旋DNA(G4-DNA)为靶点,为寻找更有效的铂类抗肿瘤药物提供新的思路。同时通过列举最新研究成果,分析药物的抗肿瘤机理及在克服顺铂耐药性机理方面的研究进展,提出铂类药物的设计研发方法,让读者了解铂类抗肿瘤药物的发展历程和未来的发展趋势。 相似文献
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Dr. Yao Zhao Dr. Julie A. Woods Dr. Nicola J. Farrer Kim S. Robinson Jitka Pracharova Dr. Jana Kasparkova Olga Novakova Huilin Li Dr. Luca Salassa Dr. Ana M. Pizarro Dr. Guy J. Clarkson Dr. Lijiang Song Prof. Dr. Viktor Brabec Prof. Dr. Peter J. Sadler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2013,19(29):9578-9591
Platinum diam(m)ine complexes, such as cisplatin, are successful anticancer drugs, but suffer from problems of resistance and side‐effects. Photoactivatable PtIV prodrugs offer the potential of targeted drug release and new mechanisms of action. We report the synthesis, X‐ray crystallographic and spectroscopic properties of photoactivatable diazido complexes trans,trans,trans‐[Pt(N3)2(OH)2(MA)(Py)] ( 1 ; MA=methylamine, Py=pyridine) and trans,trans,trans‐[Pt(N3)2(OH)2(MA)(Tz)] ( 2 ; Tz=thiazole), and interpret their photophysical properties by TD‐DFT modelling. The orientation of the azido groups is highly dependent on H bonding and crystal packing, as shown by polymorphs 1 p and 1 q . Complexes 1 and 2 are stable in the dark towards hydrolysis and glutathione reduction, but undergo rapid photoreduction with UVA or blue light with minimal amine photodissociation. They are over an order of magnitude more potent towards HaCaT keratinocytes, A2780 ovarian, and OE19 oesophageal carcinoma cells than cisplatin and show particular potency towards cisplatin‐resistant human ovarian cancer cells (A2780cis). Analysis of binding to calf‐thymus (CT), plasmids, oligonucleotide DNA and individual nucleotides reveals that photoactivated 1 and 2 form both mono‐ and bifunctional DNA lesions, with preference for G and C, similar to transplatin, but with significantly larger unwinding angles and a higher percentage of interstrand cross‐links, with evidence for DNA strand cross‐linking further supported by a comet assay. DNA lesions of 1 and 2 on a 50 bp duplex were not recognised by HMGB1 protein, in contrast to cisplatin‐type lesions. The photo‐induced platination reactions of DNA by 1 and 2 show similarities with the products of the dark reactions of the PtII compounds trans‐[PtCl2(MA)(Py)] ( 5 ) and trans‐[PtCl2(MA)(Tz)] ( 6 ). Following photoactivation, complex 2 reacted most rapidly with CT DNA, followed by 1 , whereas the dark reactions of 5 and 6 with DNA were comparatively slow. Complexes 1 and 2 can therefore give rapid potent photocytotoxicity and novel DNA lesions in cancer cells, with no activity in the absence of irradiation. 相似文献
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在反相离子对色谱中,研究了四种离子对试剂对铂络合物保留值的影响。用流动相中离子-偶极作用物和铂络合物的结构说明了保留机理。用NaCl作内标测定了顺式-二氨-1,1-环丁二羧酸铂(Ⅱ)(碳铂)和顺式二氯二氨合铂(Ⅱ)(顺铂)样品,七次配样测定得到满意的回收率,相对标准偏差分别为0.7%和0.5%,检出限为75ng/ml和0.23μg/ml。 相似文献
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Dr. Luís A. E. Batista de Carvalho Dr. M. Paula M. Marques Dr. Christine Martin Dr. Stewart F. Parker Dr. John Tomkinson 《Chemphyschem》2011,12(7):1334-1341
The well‐known platinum(II) chemotherapeutic drugs cisplatin [cis‐(NH3)2PtCl2] and carboplatin [Pt(NH3)2C6O4H6], as well as the analogous transplatin [trans‐(NH3)2PtCl2], were studied by inelastic neutron scattering (INS) spectroscopy, coupled to quantum mechanical methods, and some ancillary work with X‐ray diffraction on powders. An assignment of the experimental spectra was carried out based on the calculated INS transition frequencies and intensities (at the DFT level), thereby achieving a good correspondence between the calculated and observed data. Unusually good‐quality INS spectra were obtained from about 250 mg, which is the smallest sample of a hydrogenous compound for which a successful INS interpretation has been reported. The knowledge of the local configuration of this kind of complexes is essential for an accurate understanding of their activity, which will pave the way for the rational design of novel third‐generation drugs comprising cisplatin‐ and carboplatin‐like moieties. 相似文献
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Amal S. Basaleh Fatimah Y. Alomari Abeer A. Sharfalddin Najlaa S. Al-Radadi Doaa Domyati Mostafa A. Hussien 《Molecules (Basel, Switzerland)》2022,27(9)
Vanadium compounds have been set in various fields as anticancer, anti-diabetic, anti-parasitic, anti-viral, and anti-bacterial agents. This study reports the synthesis and structural characterization of oxidovanadium(IV)-based imidazole drug complexes by the elemental analyzer, molar conductance, magnetic moment, spectroscopic techniques, as well as thermal analysis. The obtained geometries were studied theoretically using density functional theory (DFT) under the B3LYP level. The DNA-binding nature of the ligands and their synthesized complexes has been studied by the electronic absorption titrations method. The biological studies were carried with in-vivo assays and the molecular docking method. The EPR spectra asserted the geometry around the vanadium center to be a square pyramid for metal complexes. The geometries have been confirmed using DFT under the B3LYP level. Moreover, the quantum parameters proposed promising bioactivity of the oxidovanadium(IV) complexes. The results of the DNA-binding revealed that the investigated complexes bind to DNA via non-covalent mode, and the intrinsic binding constant (Kb) value for the [VO(SO4)(MNZ)2] H2O complex was promising, which was 2.0 × 106 M−1. Additionally, the cytotoxic activity of the synthesized complexes exhibited good inhibition toward both hepatocellular carcinoma (HepG-2) and human breast cancer (HCF-7) cell lines. The results of molecular docking displayed good correlations with experimental cytotoxicity findings. Therefore, these findings suggest that our synthesized complexes can be introduced as effective anticancer agents. 相似文献
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顺 二氯一氨 (4 氨基 2 ,2 ,6 ,6 四甲基哌啶 1 氧自由基 )合铂 (Ⅱ ) (简称HJ5 )是一种有研究与应用前景的新型铂抗癌配合物。建立了常规测定HJ5含量的高效液相分析方法。流动相为V(乙腈 )∶V(水 ) =10∶90的溶液 ,检测波长为 2 10nm ,柱为PhenomenexC18(15 0mm× 3 9mmi d ,10 μm) ;采用外标法测定了HJ5的线性方程、回收率和精密度。该方法能使HJ5峰与杂质峰很好的分离 ,其峰面积与检测量呈线性关系 ,最低检出限为 0 0 7μg。用 9g/L的氯化钠水溶液作溶剂 ,能有效抑制HJ5的水解 ,使其稳定时间达到 2h以上 。 相似文献
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Mohamed M. El-bendary Tamer S. Saleh Mansour M. Alomari Ehab M. M. Ali Bambar Davaasuren Mariusz Jaremko Bandar A. Babgi 《Molecules (Basel, Switzerland)》2022,27(14)
The treatment of an aqueous acetonitrile solution of chloroplatinic acid hydrate H2PtCl6.xH2O and pyridine-2-carbaldehyde-oxime (paOH) in the presence of potassium thiocyanate at room temperature (25°) led to the formation of a new Pt(IV) complex with the formula [Pt(SCN)2(paO)2], (1). Complex 1 was fully characterized by FT-IR, UV-vis and NMR spectroscopic techniques as well as elemental analysis. The crystallographic structure of complex 1 was obtained by single-crystal X-ray diffraction. The structure of complex 1 consists of a distorted octahedral geometrical environment around the platinum center in which the coordination sites are occupied by two terminal thiocyanate ligands in trans arrangement and two bidentate paO ligands through four nitrogen atoms. In addition, the in vitro evaluation of the cytotoxicity of platinum complex 1 against four different cancer cell lines was performed. The IC50 values for colon (HCT116), liver (HepG2), breast (MCF-7) and erythroid (JK-1) treated with complex 1 are 19 ± 6, 21 ± 5, 22 ± 6, and 13 ± 3 μM, respectively. In HCT116 cells treated with the IC50 dose of our title compound, apoptosis and necrosis were increased by 34% and 27.8%, respectively. Cells halted in the proliferative phase (S phase) to 21.7 % and 29.8% in HCT116 and HepG2 cells treated with complex 1 have anti-proliferative actions. Furthermore, the catalytic activity of synthesized complex 1 was examined in the oxidation reaction of benzyl alcohols in the presence of an oxidant. Finally, the luminescence behavior of complex 1 was investigated. 相似文献